蟾毒灵平衡溶解度和表观油水分配系数的测定

目的 :测定蟾毒灵的平衡溶解度及表观油水分配系数。方法 :采用高效液相色谱(HPLC)法测定蟾毒灵在水和各种有机溶剂中的平衡溶解度,采用摇瓶法测定蟾毒灵在正辛醇-水/缓冲盐溶液中的表观油水分配系数。结果:25℃、37℃条件下,蟾毒灵平衡溶解度碱性环境下大于酸性环境,但均大于10μg/m L;蟾毒灵的溶解速度较慢,需34 h才能达到饱和。p H对蟾毒灵的表观油水分配系数影响较小,不同p H环境中,蟾毒灵log P为2.5~3.0。结论:蟾毒灵的平衡溶解度、表观油水分配系数能够满足成药性的要求。

Determination of Equilibrium Solubility and Apparent Oil-water Partition Coefficients of Bufalin

Objective:To determine equilibrium solubility and apparent oil-water partition coefficients of bufalin. Methods:High performance liquid chromatography(HPLC) method was used to determine equilibrium solubility of bufalin in water and sorts of organic solvent,and apparent oil-water partition coefficients of bufalin was determined by shake flask method in n-caprylic alcohol-water buffer salt solution. Results:Equilibrium solubility of bufalin was greater in alkaline environment than in acid environment at 25 ℃ and37 ℃,but both greater than 10 μg/m L. The solution rate of bufalin was relatively slow and it needed 34 hours to reach saturation. Apparent oil-water partition coefficients of bufalin had less effect on p H. Log P of bufalin was between 2.5 and 3.0 in different p H environment. Conclusion:Equilibrium solubility and apparent oil-water partition coefficients of bufalin are able to meet the requirements of druggability.